Process for making modulators of cystic fibrosis transmembrane conductance regulator

• US 9,751,839 B2
• Filed: 05/20/2016
• Issued: 09/05/2017
• Est. Priority Date: 03/20/2009
• Status: Active Grant

• Current Assignee: Vertex Pharmaceuticals Incorporated
• Original Assignee: Vertex Pharmaceuticals Incorporated
• Inventors: Demattei, John, Looker, Adam R., Neubert-Langille, Bobbianna, Trudeau, Martin, Roeper, Stefanie, Ryan, Michael P., Guerette, Dahrika Milfred Yap, Krueger, Brian R., Grootenhuis, Peter D. J., Van Goor, Fredrick F., Botfield, Martyn C., Zlokarnik, Gregor
• Primary Examiner(s): Rozof, Timothy R
• Application Number:
  US15/160,100
• Publication Number:
  US 20170096396A1
• Time in Patent Office: 473 Days
• Field of Search: None
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
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• CPC Class Codes: C07C 201/08 : by substitution of hydrogen atoms by nitro groups
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Abstract

The invention provides a process for the preparation of a compound of Formula 1,

comprising coupling a carboxylic acid of Formula 2

with an aniline of Formula 3

in the presence of a coupling agent.

Claims

1. A process for the preparation of a compound of Formula 1,

2. A compound of Formula 3, or a pharmaceutically acceptable salt thereof.

3. A compound of Formula 4, or a pharmaceutically acceptable salt thereof.